Page last updated: 2024-08-02 21:32:15

a-438079

Description

Cross-References

ID SourceID
PubMed CID11673921
CHEMBL ID377219
SCHEMBL ID5815398
MeSH IDM0514679

Synonyms (22)

Synonym
3-[[5-(2,3-dichlorophenyl)tetrazol-1-yl]methyl]pyridine
CHEMBL377219 ,
a-438079
a438079 ,
AKOS016035814
bdbm50410955
a 438079
HY-15488
CS-1293
NCGC00347906-01
3-((5-(2,3-dichlorophenyl)-1h-tetrazol-1-yl)methyl)pyridine
3-{[5-(2,3-dichlorophenyl)-1h-1,2,3,4-tetrazol-1-yl]methyl}pyridine
gtpl4118
MMPAULQSJLVKHP-UHFFFAOYSA-N
3-{[5-(2,3-dichlorophenyl)-1h-tetraazol-1-yl]methyl}pyridine
SCHEMBL5815398
3-[[5-(2,3-dichlorophenyl)-1h-tetrazol-1-yl]methyl]pyridine
NCGC00347906-04
3-[5-(2,3-dichloro-phenyl)-tetrazol-1-ylmethyl]-pyridine
Q27074072
HMS3748O07
MS-24422

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.2534AID1645841
GVesicular stomatitis virusPotency21.3174AID1645842
Interferon betaHomo sapiens (human)Potency21.3174AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency21.3174AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency21.3174AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency21.3174AID1645842

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)IC500.0590AID1913032; AID1913329
P2X purinoceptor 7Rattus norvegicus (Norway rat)IC500.4321AID1831763; AID266264; AID321350; AID423046; AID597637
P2X purinoceptor 7Rattus norvegicus (Norway rat)Ki0.2000AID1831767
P2X purinoceptor 7Homo sapiens (human)IC500.4830AID1358119; AID1831762; AID266262; AID321349; AID423041; AID597636
P2X purinoceptor 7Homo sapiens (human)Ki0.0680AID1831766
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.5055AID1915176
P2X purinoceptor 7Mus musculus (house mouse)IC502.9000AID1831764

Bioassays (60)

Assay IDTitleYearJournalArticle
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression2022The Journal of biological chemistry, 08, Volume: 298, Issue:8
ISSN: 1083-351X
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
ISSN: 2211-1247
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1831767Displacement of [3H]-A-804598 from rat P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
ISSN: 1520-4804
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID423041Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
ISSN: 1520-4804
Antagonists of the P2X(7) receptor. From lead identification to drug development.
AID760096Antagonist activity at P2X7 in Sprague-Dawley rat synaptosome assessed as inhibition of BzATP-induced [3H]D-aspartate efflux preincubated at 10 uM for 8 mins by liquid scintillation counting in absence of extracellular Ca2+2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
ISSN: 1948-5875
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.
AID266268Oral bioavailability in rat at 10 umol/kg, ip2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
ISSN: 0022-2623
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID266265Inhibition of ILbeta production in human THP1 cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
ISSN: 0022-2623
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID266262Antagonist activity at human P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of calcium flux by FLIPR2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
ISSN: 0022-2623
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID266266Reversal of mechanical allodynia in L5/L6 spinal nerve tight ligation model of neuropathic pain in ip dosed rat2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
ISSN: 0022-2623
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID1831766Displacement of [3H]-A-804598 from human P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
ISSN: 1520-4804
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID1831763Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
ISSN: 1520-4804
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID266264Antagonist activity at rat P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of calcium flux by FLIPR2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
ISSN: 0022-2623
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID597637Antagonist activity at rat recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
ISSN: 1464-3405
Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.
AID266263Ability to block pore formation in human THP1 cells assessed as inhibition of YO-PRO-1 diiodide dye uptake2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
ISSN: 0022-2623
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID760099Antagonist activity at P2X7 in Sprague-Dawley rat synaptosome assessed as inhibition of BzATP-induced [3H]D-aspartate efflux preincubated at 10 uM for 8 mins by liquid scintillation counting2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
ISSN: 1948-5875
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.
AID597636Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
ISSN: 1464-3405
Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.
AID423163Bioavailability in ip dosed rat2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
ISSN: 1520-4804
Antagonists of the P2X(7) receptor. From lead identification to drug development.
AID266267Reversal of mechanical allodynia in L5/L6 spinal nerve tight ligation model of neuropathic pain in ip dosed rat relative to control2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
ISSN: 0022-2623
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID321349Antagonist activity at human recombinant P2X7 receptor assessed as inhibition of BzATP-induced calcium flux by FLIPR assay2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
ISSN: 1464-3405
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
AID423164Half life in ip dosed rat2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
ISSN: 1520-4804
Antagonists of the P2X(7) receptor. From lead identification to drug development.
AID1694069Antagonist activity at P2X7R in mouse N2a cells assessed as reduction in ATP-induced calcium influx at 5 uM incubated for 1 hr by Fura-2AM dye based spectrofluorometry relative to control2021Bioorganic & medicinal chemistry, 02-01, Volume: 31ISSN: 1464-3391Synthetic 1,4-Naphthoquinones inhibit P2X7 receptors in murine neuroblastoma cells.
AID423046Activity at rat P2X7 receptor expressed in HEK cells assessed as effect on BzATP-induced ethidium uptake2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
ISSN: 1520-4804
Antagonists of the P2X(7) receptor. From lead identification to drug development.
AID321350Antagonist activity at rat recombinant P2X7 receptor assessed as inhibition of BzATP-induced calcium flux by FLIPR assay2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
ISSN: 1464-3405
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
AID266270Impairment of motor function in rat by rotarod assay up to 300 umol/kg, ip2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
ISSN: 0022-2623
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID1358119Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake2018European journal of medicinal chemistry, May-10, Volume: 151ISSN: 1768-3254
AID1831762Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
ISSN: 1520-4804
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID1831764Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
ISSN: 1520-4804
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID266269Half life in rat at 10 umol/kg2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
ISSN: 0022-2623
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID1831769Metabolic stability in human liver microsomes assessed as intrinsic clearance at 1 uM incubated for 60 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
ISSN: 1520-4804
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID1831770Metabolic stability in rat liver microsomes assessed as intrinsic clearance at 1 uM incubated for 60 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
ISSN: 1520-4804
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346612Human P2X7 (P2X receptors)2007British journal of pharmacology, Jul, Volume: 151, Issue:5
ISSN: 0007-1188
Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states.

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (25.00)29.6817
2010's5 (31.25)24.3611
2020's7 (43.75)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (87.50%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
3'-o-(4-benzoyl)benzoyladenosine 5'-triphosphatepurine ribonucleoside triphosphate2013201311.0medium000010
kn 62piperazines2009200915.0medium000100
az 116453732009200915.0medium000100
az106061202009200915.0medium000100
ce 224,535202120213.0high000001
gsk1482160202120213.0high000001
a-8399772007200717.0medium000100
jnj-47965567202120213.0medium000001
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Ache02006200717.5medium000200
Arthritis, Rheumatoid02009200915.0low000100
Chronic Disease02007200717.0low000100
Chronic Illness02007200717.0low000100
Congenital Zika Syndrome0202020204.0low000010
Disease Models, Animal0202020204.0low000010
Inflammation02007200717.0low000100
Innate Inflammatory Response02007200717.0low000100
Neuroblastoma0202120213.0low000001
Pain02006200717.5medium000200
Peripheral Nerve Diseases02006200618.0low000100
Peripheral Nervous System Diseases02006200618.0low000100
Rheumatoid Arthritis02009200915.0low000100
Zika Virus Infection0202020204.0low000010

Bioavailability (2)

ArticleYear
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8
2021
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5
2019